Phenoxypyrimidine inhibitors of p38alpha kinase: synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles |
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Authors: | Boehm J C Bower M J Gallagher T F Kassis S Johnson S R Adams J L |
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Institution: | Department of Medicinal Chemistry , GlaxoSmithKline Pharmaceuticals, King of Prussia, PA 19406, USA. jeffrey_c_boehm@sbphrd.com |
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Abstract: | As a continuation of our work with 1,4,5 substituted imidazole inhibitors of p38alpha, we report a series of 1-(4-piperidinyl)-4-(4-fluorophenyl)-5-(2-phenoxy-4-pyrimidinyl) imidazoles related to 7. The compounds have IC50's for inhibition of p38alpha ranging from 6.0 to 650nM. Statistical analysis of the p38beta inhibitor potencies shows a correlation of IC50's with the electron donating strength of low molecular weight substituents. |
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